… PROTAC technology to generate a cell-selective BCL-X L … The potent antitumor activity of
DT2216 was correlated with its … that DT2216 is a safer and more potent antitumor agent than …

… the utility of PROTAC technology to achieve tissue … activity. Compound 17b (XZ739), which
contains a PEG linker with linker length of 11 atoms, was the most potent BCL-X L degrader …

… , a potent VHL-based BCL-xL PROTAC, as a safer and more potent antitumor agent than its
… are located within the band region which is feasible to achieve a conformation that is close to …

… Thus, we have demonstrated that the PROTAC technology could be used to achieve tissue/cell
selectivity by targeting E3 ligases that are differentially expressed in different tissues/cells…

… platelets in the bloodstream until it reaches the tumor site, where it is … of degrading BCL-xL
and BCL-2 in SCLC using a single … These results suggest that 753b is a more potent antitumor …

… versus inhibition, (18−20) we report the design of a chemically distinct Bcl-xL VHL degrader,
… ternary complexation to achieve selective degradation of Bcl-xL over Bcl-2, PROTAC 6 may …

… Unlike conventional SMIs, the PROTAC molecule can be … To achieve positive cooperatively
in PROTAC strategy, the … was selectively Bcl-x L degrader but not a Bcl-2 degrader. …

… We have developed a homo-PROTAC by connecting two derivatives of … The key intermediate
12 was achieved via amide … It selectively degraded Bcl-X L and stabilized and enhanced …

… (PROTAC) derived from navitoclax, is able to overcome this on-target thrombocytopenia.
DT2216 selectively ubiquitinated and degraded … 753B is a more potent antitumor agent than …

… its activity. With DT2216 already under clinical trial as the only PROTAC degrader for BCL-xL, …
~219 min to degrade 50% of BCL-xL but 753b was unable to achieve 50% degradation …